PE20140186A1 - GLUCAGON ANALOGS PRESENTING GIP RECEPTOR ACTIVITY - Google Patents
GLUCAGON ANALOGS PRESENTING GIP RECEPTOR ACTIVITYInfo
- Publication number
- PE20140186A1 PE20140186A1 PE2013001437A PE2013001437A PE20140186A1 PE 20140186 A1 PE20140186 A1 PE 20140186A1 PE 2013001437 A PE2013001437 A PE 2013001437A PE 2013001437 A PE2013001437 A PE 2013001437A PE 20140186 A1 PE20140186 A1 PE 20140186A1
- Authority
- PE
- Peru
- Prior art keywords
- amino acid
- amino
- glucagon
- presenting
- aib
- Prior art date
Links
- MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical class C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 title abstract 4
- 230000000694 effects Effects 0.000 title abstract 2
- 150000001413 amino acids Chemical group 0.000 abstract 9
- 235000001014 amino acid Nutrition 0.000 abstract 8
- FUOOLUPWFVMBKG-UHFFFAOYSA-N 2-Aminoisobutyric acid Chemical compound CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 abstract 6
- 108010004460 Gastric Inhibitory Polypeptide Proteins 0.000 abstract 2
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 abstract 2
- -1 AMINO Chemical class 0.000 abstract 1
- 108010016626 Dipeptides Proteins 0.000 abstract 1
- 108010067722 Dipeptidyl Peptidase 4 Proteins 0.000 abstract 1
- 102100025012 Dipeptidyl peptidase 4 Human genes 0.000 abstract 1
- 102000051325 Glucagon Human genes 0.000 abstract 1
- 108060003199 Glucagon Proteins 0.000 abstract 1
- 208000011616 HELIX syndrome Diseases 0.000 abstract 1
- RAXXELZNTBOGNW-UHFFFAOYSA-O Imidazolium Chemical group C1=C[NH+]=CN1 RAXXELZNTBOGNW-UHFFFAOYSA-O 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 150000001370 alpha-amino acid derivatives Chemical class 0.000 abstract 1
- 235000008206 alpha-amino acids Nutrition 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 229960004666 glucagon Drugs 0.000 abstract 1
- 238000012986 modification Methods 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 102000014187 peptide receptors Human genes 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000001681 protective effect Effects 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- A61K38/17—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- A61K38/22—Hormones
- A61K38/26—Glucagons
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K14/00—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
- C07K14/435—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
- C07K14/575—Hormones
- C07K14/605—Glucagons
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Endocrinology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Gastroenterology & Hepatology (AREA)
- Zoology (AREA)
- Diabetes (AREA)
- Toxicology (AREA)
- Molecular Biology (AREA)
- Genetics & Genomics (AREA)
- Biophysics (AREA)
- Biochemistry (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Emergency Medicine (AREA)
- Biomedical Technology (AREA)
- Nutrition Science (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Peptides Or Proteins (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Surgical Instruments (AREA)
Abstract
SE REFIERE A UN ANALOGO DE GLUCAGON CUYA SECUENCIA DE AMINOACIDOS ES UNA DE LAS SEQ ID N�: 184 A 199, ENTRE OTROS, QUE COMPRENDE: A) UN AMINOACIDO QUE COMPRENDE UNA CADENA LATERAL DE IMIDAZOL EN LA POSICION 1 TAL COMO His O UN DERIVADO DE His; B) UN AMINOACIDO PROTECTOR DE DPP-IV EN POSICION 2 TAL COMO EL ACIDO AMINO ISOBUTIRICO (AIB); C) UN AMINOACIDO ACILADO O ALQUILADO EN LAS POSICIONES 9, 10, 12, 16, 20 O 37 A 43, EN DONDE EL GRUPO ACILO O ALQUILO ESTA LIGADO AL AMINOACIDO A TRAVES DE UN SEPARADOR QUE ES UN AMINOACIDO O UN DIPEPTIDO; D) UN AMINOACIDO QUE ESTABILIZA LA HELICE ALFA EN UNA O MAS DE LAS POSICIONES 16 A 21 QUE PUEDE SER UN AMINOACIDO CON CARGA NEGATIVA TAL COMO Glu, UN AMINOACIDO ALFA O UN a,a-DISUSTITUIDO TAL COMO AIB; E) HASTA 10 MODIFICACIONES DE AMINOACIDO EN RELACION CON LA SECUENCIA DE AMINOACIDOS DEL GLUCAGON DE SEQ ID N�: 1; EN DONDE EL ANALOGO DE GLUCAGON PRESENTA UNA ACTIVIDAD MEJORADA SOBRE EL RECEPTOR DEL PEPTIDO INSULINOTROPICO DEPENDIENTE DE GLUCOSA (GIP). TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA UTIL EN EL TRATAMIENTO DE DIABETES, OBESIDADIT REFERS TO A GLUCAGON ANALOGUE WHOSE AMINO ACID SEQUENCE IS ONE OF SEQ ID N�: 184 TO 199, AMONG OTHERS, WHICH INCLUDES: A) AN AMINO ACID THAT INCLUDES A SIDE CHAIN OF IMIDAZOLE IN POSITION 1 SUCH AS His OR A DERIVED FROM His; B) A PROTECTIVE AMINO ACID OF DPP-IV IN POSITION 2 SUCH AS AMINO ISOBUTYRIC ACID (AIB); C) AN AMINO ACIL OR RENTED IN POSITIONS 9, 10, 12, 16, 20 OR 37 TO 43, WHERE THE ACILO OR RENT GROUP IS LINKED TO THE AMINO ACID THROUGH A SEPARATOR THAT IS AN AMINO ACID OR A DIPEPTIDE; D) AN AMINO ACID THAT STABILIZES THE ALPHA HELIX IN ONE OR MORE OF POSITIONS 16 TO 21 WHICH MAY BE AN AMINO ACID WITH NEGATIVE CHARGE SUCH AS Glu, AN ALPHA AMINO ACID OR AN a, a-DISUSTITUTED SUCH AS AIB; E) UP TO 10 AMINO ACID MODIFICATIONS IN RELATION TO THE SEQUENCE OF AMINO ACIDS OF THE GLUCAGON OF SEQ ID N�: 1; WHERE THE GLUCAGON ANALOGUE PRESENTS AN IMPROVED ACTIVITY ON THE GLUCOSE-DEPENDENT INSULINOTROPIC PEPTIDE RECEPTOR (GIP). ALSO REFERS TO A USEFUL PHARMACEUTICAL COMPOSITION IN THE TREATMENT OF DIABETES, OBESITY
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201061426285P | 2010-12-22 | 2010-12-22 | |
| US201161514609P | 2011-08-03 | 2011-08-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20140186A1 true PE20140186A1 (en) | 2014-02-13 |
Family
ID=45476658
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2013001437A PE20140186A1 (en) | 2010-12-22 | 2011-12-20 | GLUCAGON ANALOGS PRESENTING GIP RECEPTOR ACTIVITY |
Country Status (22)
| Country | Link |
|---|---|
| US (4) | US8507428B2 (en) |
| EP (1) | EP2654773B1 (en) |
| JP (1) | JP6086067B2 (en) |
| KR (1) | KR20130132931A (en) |
| CN (1) | CN103458920B (en) |
| AR (1) | AR084459A1 (en) |
| AU (1) | AU2011349331A1 (en) |
| BR (1) | BR112013015389A2 (en) |
| CA (1) | CA2821766A1 (en) |
| CL (1) | CL2013001783A1 (en) |
| CO (1) | CO6761302A2 (en) |
| CR (1) | CR20130295A (en) |
| EA (1) | EA201390941A1 (en) |
| EC (1) | ECSP13012697A (en) |
| ES (1) | ES2713952T3 (en) |
| MA (1) | MA34885B1 (en) |
| MX (1) | MX2013006304A (en) |
| NZ (1) | NZ612297A (en) |
| PE (1) | PE20140186A1 (en) |
| PH (1) | PH12013501215A1 (en) |
| SG (1) | SG191194A1 (en) |
| WO (1) | WO2012088116A2 (en) |
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| CN103458920B (en) * | 2010-12-22 | 2016-07-06 | 印第安那大学科技研究公司 | Show the glucagon analogs of GIP receptor active |
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| EP2758426B1 (en) | 2011-09-23 | 2019-08-07 | Novo Nordisk A/S | Novel glucagon analogues |
| CN104583232B (en) | 2012-06-21 | 2018-04-13 | 印第安纳大学研究及科技有限公司 | Show the glucagon analogs of GIP receptor actives |
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- 2011-12-20 US US13/331,816 patent/US8507428B2/en not_active Expired - Fee Related
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- 2013-06-18 CO CO13145190A patent/CO6761302A2/en unknown
- 2013-06-18 CL CL2013001783A patent/CL2013001783A1/en unknown
- 2013-06-18 CR CR20130295A patent/CR20130295A/en not_active Application Discontinuation
- 2013-06-18 EC ECSP13012697 patent/ECSP13012697A/en unknown
-
2015
- 2015-03-23 US US14/665,508 patent/US20150259393A1/en not_active Abandoned
- 2015-12-28 US US14/981,187 patent/US9587005B2/en active Active
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| MX2013006304A (en) | 2013-07-02 |
| US9249206B2 (en) | 2016-02-02 |
| KR20130132931A (en) | 2013-12-05 |
| CR20130295A (en) | 2013-10-09 |
| EP2654773B1 (en) | 2018-10-03 |
| JP6086067B2 (en) | 2017-03-01 |
| PH12013501215A1 (en) | 2013-11-18 |
| BR112013015389A2 (en) | 2016-11-22 |
| ES2713952T3 (en) | 2019-05-24 |
| MA34885B1 (en) | 2014-02-01 |
| CA2821766A1 (en) | 2012-06-28 |
| WO2012088116A3 (en) | 2012-11-15 |
| US9587005B2 (en) | 2017-03-07 |
| US20120238493A1 (en) | 2012-09-20 |
| CN103458920A (en) | 2013-12-18 |
| US20130116173A1 (en) | 2013-05-09 |
| JP2014507402A (en) | 2014-03-27 |
| WO2012088116A2 (en) | 2012-06-28 |
| AR084459A1 (en) | 2013-05-15 |
| US8507428B2 (en) | 2013-08-13 |
| CO6761302A2 (en) | 2013-09-30 |
| NZ612297A (en) | 2015-10-30 |
| CN103458920B (en) | 2016-07-06 |
| US20150259393A1 (en) | 2015-09-17 |
| SG191194A1 (en) | 2013-07-31 |
| ECSP13012697A (en) | 2013-10-31 |
| CL2013001783A1 (en) | 2014-01-24 |
| EP2654773A2 (en) | 2013-10-30 |
| US20160115215A1 (en) | 2016-04-28 |
| EA201390941A1 (en) | 2013-12-30 |
| AU2011349331A1 (en) | 2013-07-11 |
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